5-HT Receptor Antagonists Information Drug – Precautions and Side Effects
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Type of Drug:

Antinauseants; antiemetics; drugs used to prevent nausea and vomiting.

How the Drug Works:

Dolasetron, granisetron, and ondansetron are selective serotonin 5-HT 3 receptor antagonists that block serotonin stimulation to prevent nausea and vomiting.


Oral doseforms - To prevent nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemstherapy.

Oral dolasetron and ondansetron - To prevent postoperative nausea and vomiting.

Oral granisetron and ondansetron - To prevent nausea and vomiting associated with radiotherapy in patients receiving either total body irradiation, single high-dose fraction, or daily fractions the abdomen.

Intravenous (IV; into a vein) dolasetron - To prevent and treat postoperative nausea or vomiting.

Unlabeled Uses: Dolasetron has been used to treat radiotherapy-induced nausea and vomiting. Granisetron has been used for acute nausea and vomiting following surgery. Ondansetron has been used in the treatment of nausea and vomiting associated with acetaminophen poisoning, acute levodopa-induced psychosis, and prostacyclin therapy; to reduce bulimic episodes in patients with bulimia nervosa; to treat patients with social anxiety disorder; and as treatment of spinal or epidural morphine-induced pruritis.


Benzyl alcohol: Some of these products contain benzyl alcohol, which has been associated with a fatal “gasping syndrome” in premature infants. Consult your doctor or pharmacist.

Phenylketonuria: Ondansetron orally-disintegrating tablets contain phenylalanine. Consult your doctor or pharmacist.

Pregnancy: There are no adequate and well-controlled studies in pregnant women. Use only if clearly needed and the potential benefits to the mother outweigh the possible hazards to the fetus.

Breastfeeding: Ondansetron appears in breast milk. It is not known if other 5-HT 3 receptor antagonists appear in breast milk. Consult your doctor before you begin breastfeeding.

Children: Safety and effectiveness for use of dolasetron and the injection form of granisetron in children younger than 2 years of age have not been established. Safety and effectiveness for use of the oral form of granisetron in children of any age have not been established. Safety and effectiveness for use of ondansetron in children 3 years of age and younger have not been established.

Drug Interactions:

Tell your doctor or pharmacist if you are taking or if you are planning to take any over-the-counter or prescription medications or dietary supplolnol1ls while taking a 5-HT 3 receptor antagonist. Doses of one or both drugs may need to be modified or a different drug may need to be prescribrd. Rifamycins (eg, rifampin) interact with ondansetron

Side Effects:

Every drug is capable of producing side effects. Many 5-HT 3 receptor antagonist users experience no, or minor, side effects. The frequency and severity of side effects depend on many factors including dose, duration of therapy, and individual susceptibility. Possible side effects include:

Digestive Tract: Diarrhea; nausea; constipation; stomach pain; appetite loss; taste disorder; indigestion; dry mouth.

Nervous System: Headache; drowsiness; weakness; agitation; fatigue; anxiety; stimulation; sleeplessness; dizziness; flushing; shivers; chills; vertigo (feeling of whirling motion); agitation.

Other: Changes in blood pressure; fever; heart rhythm changes; hair loss; abnormal blood counts; muscle, joint, chest, or bone pain; general body discomfort; injection site reaction; cold sensation; rash; tremor; itching; urinary retention; tingling or prickling sensation; deficient oxygenation of the blood.

Guidelines for Use:

  • Dosage is individualized. Take exactly as prescribed.
  • Do not change the dose or stop taking, unless advised by your doctor.
  • Ondansetron orally-disintegrating tablets – Remove the tablets from the package just before taking. Peel backing off blister and remove tab­let gently. Place tablet on the tongue and swallow with saliva. Tablets disintegrate rapidly on the tongue and do not require water for dissolution or swallowing.
  • Contact your doctor immediately if you experience rash, itching, short­ness of breath, abnormal heart rhythm, dizziness, fainting, low blood pressure, hives, facial swelling, or difficulty breathing.
  • Dolasetron injection can be mixed in apple or apple-grape juice and given orally. The mixed product may be kept up to 2 hours at room temperature (59 to 86°F).
  • Store at controlled room temperature (68 to 77°F). Protect from light. Do not freeze injection vials.

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